Novel P2X7 receptor antagonists |
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| Authors: | Alcaraz L Baxter A Bent J Bowers K Braddock M Cladingboel D Donald D Fagura M Furber M Laurent C Lawson M Mortimore M McCormick M Roberts N Robertson M |
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| Affiliation: | Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK. alcaraz@astrazeneca.com |
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| Abstract: | The synthesis and pharmacological evaluation of a new series of potent P2X(7) receptor antagonists is disclosed. The compounds inhibit BzATP-mediated pore formation in THP-1 cells. The distribution of the P2X(7) receptor in inflammatory cells, most notably the macrophage, mast cell and lymphocyte, suggests that P2X(7) antagonists have a significant role to play in the treatment of inflammatory disease. |
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